TY - JOUR T1 - Potential of guggulsterone, a farnesoid X receptor antagonist, in the prevention and treatment of cancer A1 - Girisa, Sosmitha A1 - Parama, Dey A1 - Harsha, Choudhary A1 - Banik, Kishore A1 - Kunnumakkara, Ajaikumar B Y1 - 2020/// KW - anticancer activities KW - cancer KW - commiphora wightii KW - guggulsterone KW - z and e isomers JF - Exploration of Targeted Anti-tumor Therapy VL - 1 IS - 5 SP - 313 EP - 342 DO - 10.37349/etat.2020.00019 UR - https://www.explorationpub.com/Journals/etat/Article/10019 N2 - Cancer is one of the most dreadful diseases in the world with a mortality of 9.6 million annually. Despite the advances in diagnosis and treatment during the last couple of decades, it still remains a serious concern due to the limitations associated with currently available cancer management strategies. Therefore, alternative strategies are highly required to overcome these glitches. The importance of medicinal plants as primary healthcare has been well-known from time immemorial against various human diseases, including cancer. Commiphora wightii that belongs to Burseraceae family is one such plant which has been used to cure various ailments in traditional systems of medicine. This plant has diverse pharmacological properties such as antioxidant, antibacterial, antimutagenic, and antitumor which mostly owes to the presence of its active compound guggulsterone (GS) that exists in the form of Z- and E-isomers. Mounting evidence suggests that this compound has promising anticancer activities and was shown to suppress several cancer signaling pathways such as NF-κB/ERK/MAPK/AKT/STAT and modulate the expression of numerous signaling molecules such as the farnesoid X receptor, cyclin D1, survivin, caspases, HIF-1α, MMP-9, EMT proteins, tumor suppressor proteins, angiogenic proteins, and apoptotic proteins. The current review is an attempt to summarize the biological activities and diverse anticancer activities (both in vitro and in vivo) of the compound GS and its derivatives, along with its associated mechanism against various cancers. ER -